GO-Y078
GO-Y078 is a curcumin (HY-N0005) analog. GO-Y078 activates p38/JNK1/2. GO-Y078 activates the MAPK pathway, Caspase 3/8/9, PARP, AP-1, DR5, and TP53, while inhibiting cIAP-1, XIAP, and NF-κB. GO-Y078 induces sub-G1/G2/M phase arrest and Apoptosis. GO-Y078 impairs angiogenesis. GO-Y078 can be used in research related to osteosarcoma, cervical cancer, oral squamous cell carcinoma, and peritoneal metastasis of gastric cancer.
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- CAS No.: 1217503-60-0
- 화학식: C22H24O7
- 분자량:400.43
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
[1]|
cIAP-1 |
XIAP |
Caspase 3 |
Caspase 8 |
Caspase 9 |
JNK1 |
JNK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SiHa | IC50 |
7.76 μM
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Inhibition of cell viability against human cervical squamous cell carcinoma SiHa cells assessed via MTT-based colorimetric assay after 24 h incubation.
Inhibition of cell viability against human cervical squamous cell carcinoma SiHa cells assessed via MTT-based colorimetric assay after 24 h incubation.
|
42059340 |
| HeLa | IC50 |
11.94 μM
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Inhibition of cell viability against human cervical adenocarcinoma HeLa cells assessed via MTT-based colorimetric assay after 24 h incubation.
Inhibition of cell viability against human cervical adenocarcinoma HeLa cells assessed via MTT-based colorimetric assay after 24 h incubation.
|
42059340 |
In Vitro
GO-Y078 (1-16 μM; 24 h) reduces the viability of osteosarcoma U2OS, MG-63, 143B and Saos-2 cells in a dose-dependent manner. After 24 h of treatment, the inhibitory effect is the strongest at the concentration of 16 μM (the viability of U2OS cells decreases by 54.7%, that of MG-63 cells by 79.6%, that of 143B cells by 58.9%, and that of Saos-2 cells by 71.6%)[1].
GO-Y078 (2.5-40 μM; 24 h) inhibits the viability of cervical squamous cell carcinoma SiHa cells and cervical adenocarcinoma HeLa cells, with an IC50 of 7.76 μM for the former and 11.94 μM for the latter[2].
GO-Y078 (0.5-4 μM; 24 h) potently inhibits the viability of SCC-9 and HSC-3 oral squamous cell carcinoma cells, with an IC50 of <4 μM, and exhibits stronger cytotoxic potency than DMC[3].
GO-Y078 (1-8 μM; 24 h) induces sub-G1 phase cell cycle arrest in osteosarcoma U2OS and 143B cells. After treatment with 8 μM for 24 h, the proportion of sub-G1 phase cells increases to 24.3% in U2OS cells and to 26.9% in 143B cells[1].
GO-Y078 (1-8 μM; 24 h) induces apoptosis in osteosarcoma U2OS and 143B cells in a dose-dependent manner. After 24 h of treatment, the proportion of Annexin V-positive cells increases to approximately 35% in U2OS cells and to approximately 50% in 143B cells at the concentration of 8 μM[1].
GO-Y078 (1-8 μM; 24 h) reduces the expression of anti-apoptotic proteins cIAP-1 and XIAP in osteosarcoma U2OS and 143B cells in a dose-dependent manner, while upregulating the level of pro-apoptotic activated caspase-3 in U2OS cells after 24 h of treatment[1].
GO-Y078 (1-8 μM; 24 h) activates the ERK1/2, JNK1/2 and p38 MAPK signaling pathways in osteosarcoma U2OS and 143B cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human osteosarcoma U2OS, MG-63, 143B, and Saos-2 cells
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Concentration:1-16 μM
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Incubation Time:24 h
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Result:Reduced cell viability in a dose-dependent manner across all four cell lines.
Reduced U2OS cell viability by 41.5% at 8 μM and 54.7% at 16 μM.
Reduced MG-63 cell viability by 39.9% at 8 μM and 79.6% at 16 μM.
Reduced 143B cell viability by 51.8% at 8 μM and 58.9% at 16 μM.
Reduced Saos-2 cell viability by 57.4% at 8 μM and 71.6% at 16 μM.
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Cell Line:human osteosarcoma U2OS and 143B cells
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Concentration:1-8 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent increase in the sub-G1 cell fraction in both cell lines.
Increased U2OS sub-G1 fraction from 4.7% (control) to 24.3% at 8 μM.
Increased 143B sub-G1 fraction from 5.2% (control) to 26.9% at 8 μM.
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Cell Line:human osteosarcoma U2OS and 143B cells
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Concentration:1-8 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent increase in total Annexin V-positive (early + late apoptotic) cells in both cell lines.
Increased U2OS Annexin V-positive cells to ~35% at 8 μM.
Increased 143B Annexin V-positive cells to ~50% at 8 μM.
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Cell Line:human osteosarcoma U2OS and 143B cells
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Concentration:8 μM (apoptosis array); 1-8 μM (Western blot)
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Incubation Time:24 h (apoptosis array); 24 h (Western blot)
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Result:Increased cleaved caspase-3 levels and decreased cIAP-1 and XIAP levels in U2OS cells at 8 μM (apoptosis array).
Caused dose-dependent reductions in cIAP-1 and XIAP expression in both U2OS and 143B cells.
Reduced U2OS cIAP-1 to near 0% and XIAP to near 10% of control levels at 8 μM.
Reduced 143B cIAP-1 to ~20% and XIAP to ~40% of control levels at 8 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KSN/Slc (nu/nu) (6-week-old male, peritoneal carcinomatosis model established by intraperitoneal inoculation of GCIY gastric cancer cells)[5]
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Dosage:133 mg/kg; 266 mg/kg
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Administration:i.p.
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Result:Suppressed ascites fluid accumulation completely, with average body weight of 29.1 g at 17 days after first treatment.
Increased median survival time to 30.5 days, representing an approximate 40% increase in survival time.
Extended survival time range to 25 to 109 days.
Chemical Information
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CAS No. 1217503-60-0
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분자량 400.43
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화학식 C22H24O7
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SMILES
O(C)C1=C(OC)C(OC)=CC(/C=C/C(/C=C/C2=CC(OC)=C(O)C(OC)=C2)=O)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- GO-Y078
- 1217503-60-0
- Drug Derivative
- p38 MAPK
- JNK
- Caspase
- PARP
- AP-1
- TNF Receptor
- MDM-2/p53
- IAP
- NF-κB
- Apoptosis
- MAPK pathway
- oral squamous cell carcinoma
- human osteosarcoma U2OS cells
- human cervical squamous cell carcinoma SiHa cells
- osteosarcoma
- p38
- cell cycle arrest
- JNK1/2
- apoptosis
- cervical cancer
- Inhibitor
- inhibitor
- inhibit